HRP20180916T1 - Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use - Google Patents
Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use Download PDFInfo
- Publication number
- HRP20180916T1 HRP20180916T1 HRP20180916TT HRP20180916T HRP20180916T1 HR P20180916 T1 HRP20180916 T1 HR P20180916T1 HR P20180916T T HRP20180916T T HR P20180916TT HR P20180916 T HRP20180916 T HR P20180916T HR P20180916 T1 HRP20180916 T1 HR P20180916T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- phenyl
- trans
- compound according
- cyclopropylamino
- Prior art date
Links
- 101000615488 Homo sapiens Methyl-CpG-binding domain protein 2 Proteins 0.000 title 1
- 102100021299 Methyl-CpG-binding domain protein 2 Human genes 0.000 title 1
- 101100334370 Schizosaccharomyces pombe (strain 972 / ATCC 24843) fas2 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 37
- 208000012902 Nervous system disease Diseases 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 208000025966 Neurological disease Diseases 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- XBBRLCXCBCZIOI-DLBZAZTESA-N vafidemstat Chemical compound O1C(N)=NN=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 XBBRLCXCBCZIOI-DLBZAZTESA-N 0.000 claims 5
- -1 C-amido Chemical group 0.000 claims 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003368 amide group Chemical group 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000004202 carbamide Substances 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000006317 cyclopropyl amino group Chemical group 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 150000003456 sulfonamides Chemical class 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- RAIPHJJURHTUIC-UHFFFAOYSA-N 1,3-thiazol-2-amine Chemical compound NC1=NC=CS1 RAIPHJJURHTUIC-UHFFFAOYSA-N 0.000 claims 1
- MCRPCHPLDTWWIQ-ZWKOTPCHSA-N 3-[4-[(1s,2r)-2-[(2-amino-1,3-thiazol-5-yl)methylamino]cyclopropyl]phenyl]phenol Chemical compound S1C(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(O)C=CC=2)C1 MCRPCHPLDTWWIQ-ZWKOTPCHSA-N 0.000 claims 1
- LHGWKSSSHJWPDK-RBUKOAKNSA-N 3-[4-[(1s,2r)-2-[(2-aminopyrimidin-5-yl)methylamino]cyclopropyl]phenyl]phenol Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(O)C=CC=2)C1 LHGWKSSSHJWPDK-RBUKOAKNSA-N 0.000 claims 1
- QNMAQELYEAAQOX-DOTOQJQBSA-N 3-[5-[(1s,2r)-2-[(2-amino-1,3-thiazol-5-yl)methylamino]cyclopropyl]pyridin-2-yl]phenol Chemical compound S1C(N)=NC=C1CN[C@H]1[C@H](C=2C=NC(=CC=2)C=2C=C(O)C=CC=2)C1 QNMAQELYEAAQOX-DOTOQJQBSA-N 0.000 claims 1
- HQKNDJJROYDZDO-FUHWJXTLSA-N 3-[5-[(1s,2r)-2-[(2-aminopyrimidin-5-yl)methylamino]cyclopropyl]pyridin-2-yl]phenol Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=NC(=CC=2)C=2C=C(O)C=CC=2)C1 HQKNDJJROYDZDO-FUHWJXTLSA-N 0.000 claims 1
- VJOTYGQWNUGGSP-DLBZAZTESA-N 5-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]-1,2,4-oxadiazol-3-amine Chemical compound NC1=NOC(CN[C@H]2[C@@H](C2)C=2C=CC(OCC=3C=CC=CC=3)=CC=2)=N1 VJOTYGQWNUGGSP-DLBZAZTESA-N 0.000 claims 1
- UKYBJIFGAZGUOR-RBUKOAKNSA-N 5-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]-1,3-thiazol-2-amine Chemical compound S1C(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 UKYBJIFGAZGUOR-RBUKOAKNSA-N 0.000 claims 1
- HJWZUPRHNBJKHE-VQTJNVASSA-N 5-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]pyrimidin-2-amine Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 HJWZUPRHNBJKHE-VQTJNVASSA-N 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 230000007419 viral reactivation Effects 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
- C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
- C07D253/06—1,2,4-Triazines
- C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
- C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members with hetero atoms, or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D261/14—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/28—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/48—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
- C07D271/07—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
- C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/40—Unsubstituted amino or imino radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
- C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
- C07D285/135—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Claims (29)
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP10171342 | 2010-07-29 | ||
EP11160731 | 2011-03-31 | ||
EP11160728 | 2011-03-31 | ||
EP11160738 | 2011-03-31 | ||
EP11749119.1A EP2598482B1 (en) | 2010-07-29 | 2011-07-27 | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
PCT/EP2011/062949 WO2012013728A1 (en) | 2010-07-29 | 2011-07-27 | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20180916T1 true HRP20180916T1 (en) | 2018-08-10 |
Family
ID=44514682
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20180916TT HRP20180916T1 (en) | 2010-07-29 | 2018-06-12 | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
Country Status (24)
Country | Link |
---|---|
US (3) | US9181198B2 (en) |
EP (2) | EP2598482B1 (en) |
JP (2) | JP6054868B2 (en) |
KR (1) | KR101866858B1 (en) |
CN (2) | CN103124724B (en) |
AU (1) | AU2011284688B2 (en) |
CA (1) | CA2806008C (en) |
CY (1) | CY1120586T1 (en) |
DK (1) | DK2598482T3 (en) |
ES (1) | ES2674747T3 (en) |
HR (1) | HRP20180916T1 (en) |
HU (1) | HUE037937T2 (en) |
IL (1) | IL224389A (en) |
LT (1) | LT2598482T (en) |
ME (1) | ME03085B (en) |
MX (1) | MX341732B (en) |
NO (1) | NO2598482T3 (en) |
PL (1) | PL2598482T3 (en) |
PT (1) | PT2598482T (en) |
RS (1) | RS57331B1 (en) |
RU (1) | RU2611437C2 (en) |
SI (1) | SI2598482T1 (en) |
TR (1) | TR201809057T4 (en) |
WO (1) | WO2012013728A1 (en) |
Families Citing this family (77)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010043721A1 (en) | 2008-10-17 | 2010-04-22 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
EP2389362B1 (en) | 2009-01-21 | 2019-12-11 | Oryzon Genomics, S.A. | Phenylcyclopropylamine derivatives and their medical use |
EP2480528B1 (en) | 2009-09-25 | 2018-08-29 | Oryzon Genomics, S.A. | Lysine specific demethylase-1 inhibitors and their use |
WO2011042217A1 (en) | 2009-10-09 | 2011-04-14 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
US9616058B2 (en) | 2010-02-24 | 2017-04-11 | Oryzon Genomics, S.A. | Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use |
US9186337B2 (en) | 2010-02-24 | 2015-11-17 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae |
HUE030938T2 (en) * | 2010-04-19 | 2017-06-28 | Oryzon Genomics Sa | Lysine specific demethylase-1 inhibitors and their use |
WO2012013728A1 (en) | 2010-07-29 | 2012-02-02 | Oryzon Genomics S.A. | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
EP2598480B1 (en) | 2010-07-29 | 2019-04-24 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
US9061966B2 (en) * | 2010-10-08 | 2015-06-23 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
EP2712316A1 (en) | 2011-02-08 | 2014-04-02 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
EP3981395A1 (en) | 2011-02-08 | 2022-04-13 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
SG193241A1 (en) | 2011-03-25 | 2013-10-30 | Glaxosmithkline Ip No 2 Ltd | Cyclopropylamines as lsd1 inhibitors |
WO2012156531A2 (en) | 2011-05-19 | 2012-11-22 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for inflammatory diseases or conditions |
US20140296255A1 (en) | 2011-05-19 | 2014-10-02 | Oryzong Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
EP2768805B1 (en) | 2011-10-20 | 2020-03-25 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
IL264982B (en) | 2011-10-20 | 2022-08-01 | Oryzon Genomics Sa | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
CN105051005B (en) * | 2012-10-12 | 2017-06-13 | 武田药品工业株式会社 | Cyclopropylamine compound and application thereof |
CN102863341B (en) * | 2012-10-22 | 2014-05-07 | 南通大学 | Chemical synthesis method of (1R, 2S)-2-aryl cyclopropylamine derivative |
EP2740474A1 (en) | 2012-12-05 | 2014-06-11 | Instituto Europeo di Oncologia S.r.l. | Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
US9918983B2 (en) * | 2013-05-30 | 2018-03-20 | The Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas | Suicidal LSD1 inhibitors targeting SOX2-expressing cancer cells |
MX2016001587A (en) | 2013-08-06 | 2016-08-05 | Imago Biosciences Inc | Kdm1a inhibitors for the treatment of disease. |
DK3105218T3 (en) | 2014-02-13 | 2019-11-04 | Incyte Corp | CYCLOPROPYLAMINES AS LSD1 INHIBITORS |
WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
WO2015123408A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
EA201691594A1 (en) | 2014-02-13 | 2017-02-28 | Инсайт Корпорейшн | CYCLOPROPYLAMINES AS LSD1 INHIBITORS |
MX2016013369A (en) | 2014-04-11 | 2017-02-09 | Takeda Pharmaceuticals Co | Cyclopropanamine compound and use thereof. |
US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
TWI687419B (en) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | Imidazopyridines and imidazopyrazines as LSD1 inhibitors |
WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
CN107106517A (en) | 2014-08-25 | 2017-08-29 | 堪培拉大学 | Composition for adjusting cancer stem cell and application thereof |
EA039196B1 (en) * | 2014-10-08 | 2021-12-16 | Инсайт Корпорейшн | Cyclopropylamines as lsd1 inhibitors |
EP3250552B1 (en) * | 2015-01-30 | 2019-03-27 | Genentech, Inc. | Therapeutic compounds and uses thereof |
BR112017017074A2 (en) | 2015-02-12 | 2018-04-10 | Imago Biosciences Inc | COMPOUNDS; SALT; N - ((S) -5 - ((1R, 2S) -2- (4-FLUOROFENYL) CYCLOPROPYLAMINE) -1- (4-METHYLPIPERAZIN-1- IL) -1-OXOPENTAN-2-IL) BIS-TOSILATES -4- (1H-1,2,3-TRIAZOL-1-IL) BENZAMIDE; TOSILATE SALT OF A COMPOUND; BIS-TOSILATE SALT OF A COMPOUND; COMPOUNDS, SALTS, POLYMORPHES OR SOLVATES; PHARMACEUTICAL COMPOSITIONS, METHOD FOR KDM1A INHIBITION; METHODS FOR TREATING A DISEASE MEDIATED BY KDM1A OR GLOBINE; METHOD TO ACHIEVE AN EFFECT ON A PATIENT; METHOD FOR INHIBIT AT LEAST ONE KDM1A FUNCTION |
US9944647B2 (en) | 2015-04-03 | 2018-04-17 | Incyte Corporation | Heterocyclic compounds as LSD1 inhibitors |
EP3090998A1 (en) | 2015-05-06 | 2016-11-09 | F. Hoffmann-La Roche AG | Solid forms |
CN107849611A (en) * | 2015-06-12 | 2018-03-27 | 奥瑞泽恩基因组学股份有限公司 | Biomarker related to LSD1 inhibitor and application thereof |
WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
TWI765860B (en) | 2015-08-12 | 2022-06-01 | 美商英塞特公司 | Salts of an lsd1 inhibitor |
WO2017079476A1 (en) | 2015-11-05 | 2017-05-11 | Mirati Therapeutics, Inc. | Lsd1 inhibitors |
AU2016360481B2 (en) | 2015-11-27 | 2019-09-12 | Taiho Pharmaceutical Co., Ltd. | Novel biphenyl compound or salt thereof |
WO2017109061A1 (en) * | 2015-12-23 | 2017-06-29 | Ieo - Istituto Europeo Di Oncologia S.R.L. | Spirocyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
CA3009805C (en) | 2015-12-29 | 2023-10-17 | Mirati Therapeutics, Inc. | Lsd1 inhibitors |
CN107176927B (en) * | 2016-03-12 | 2020-02-18 | 福建金乐医药科技有限公司 | Histone demethylase LSD1 inhibitors |
SG10201913290QA (en) | 2016-03-15 | 2020-03-30 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for the treatment of hematological malignancies |
SG10201913331VA (en) | 2016-03-15 | 2020-03-30 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of solid tumors |
CN107200706A (en) * | 2016-03-16 | 2017-09-26 | 中国科学院上海药物研究所 | Cyclopropylamine class compound of one class fluorine substitution and preparation method thereof, pharmaceutical composition and purposes |
JP2019512546A (en) * | 2016-03-16 | 2019-05-16 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Methods for determining KDM1A target association, and chemical probes useful therefor |
BR112018071585B1 (en) | 2016-04-22 | 2024-01-02 | Incyte Corporation | FORMULATIONS OF AN LSD1 INHIBITOR, THEIR USES AND METHOD OF PREPARATION THEREOF |
CA2988220C (en) | 2016-06-10 | 2021-03-02 | Oryzon Genomics, S.A. | Methods of treating multiple sclerosis |
CN111194306B (en) | 2016-08-16 | 2023-05-16 | 伊美格生物科学公司 | Methods and processes for preparing KDM1A inhibitors |
EP3535420A1 (en) | 2016-11-03 | 2019-09-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
WO2018091691A1 (en) * | 2016-11-17 | 2018-05-24 | Cytoo | Lsd1 inhibitors as skeletal muscle hypertrophy inducers |
US20200069677A1 (en) | 2016-12-09 | 2020-03-05 | Constellation Pharmaceuticals, Inc. | Markers for personalized cancer treatment with lsd1 inhibitors |
WO2018137644A1 (en) * | 2017-01-24 | 2018-08-02 | 南京明德新药研发股份有限公司 | Lsd1 inhibitor and preparation method and application thereof |
MA50466A (en) | 2017-05-26 | 2020-09-02 | Taiho Pharmaceutical Co Ltd | NEW BIPHENYL COMPOUND OR SALT |
EP3632443B1 (en) | 2017-05-26 | 2023-06-07 | Taiho Pharmaceutical Co., Ltd. | Anti-tumor effect potentiator using a biphenyl compound |
AU2018276611B2 (en) * | 2017-05-31 | 2022-01-06 | Taiho Pharmaceutical Co., Ltd. | Method for predicting therapeutic effect of LSD1 inhibitor based on expression of INSM1 |
JP2020152641A (en) * | 2017-07-07 | 2020-09-24 | 国立研究開発法人理化学研究所 | Novel compound having lysine-specific demethylating enzyme 1 inhibitory activity, method for producing the same, and use of the same |
SG11202000077RA (en) * | 2017-08-03 | 2020-02-27 | Oryzon Genomics Sa | Methods of treating behavior alterations |
WO2019068326A1 (en) | 2017-10-05 | 2019-04-11 | Université D'aix-Marseille | Lsd1 inhibitors for the treatment and prevention of cardiomyopathies |
AU2019265022A1 (en) | 2018-05-11 | 2021-01-07 | Imago Biosciences, Inc. | KDM1A inhibitors for the treatment of disease |
KR20210034058A (en) | 2018-07-20 | 2021-03-29 | 씨에스피씨 종콰이 팔마씨우티컬 테크놀로지 (스자좡) 컴퍼니 리미티드 | Salts of LSD1 inhibitors and crystalline forms thereof |
US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
WO2020052647A1 (en) * | 2018-09-13 | 2020-03-19 | 南京明德新药研发有限公司 | Spiro-heterocyclic compound acting as lsd1 inhibitor and use thereof |
EP3941465A1 (en) | 2019-03-20 | 2022-01-26 | Oryzon Genomics, S.A. | Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat |
KR20210141933A (en) | 2019-03-20 | 2021-11-23 | 오리존 지노믹스 에스.에이. | How to treat borderline personality disorder |
CN114341366A (en) | 2019-07-05 | 2022-04-12 | 奥莱松基因组股份有限公司 | Biomarkers and methods for personalized treatment of small cell lung cancer using KDM1A inhibitors |
EP4025210A1 (en) | 2019-09-03 | 2022-07-13 | Oryzon Genomics, S.A. | Vafidemstat for use in treating autism spectrum disorders |
WO2021228146A1 (en) * | 2020-05-12 | 2021-11-18 | 石药集团中奇制药技术(石家庄)有限公司 | Use of lsd1 inhibitor |
EP3964204A1 (en) | 2020-09-08 | 2022-03-09 | Université d'Aix-Marseille | Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues |
WO2022214303A1 (en) | 2021-04-08 | 2022-10-13 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for treating myeloid cancers |
CN113582906B (en) * | 2021-08-24 | 2023-05-16 | 郑州大学 | Difluoro benzphetamine compound and preparation method and application thereof |
WO2023217758A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
WO2023217784A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
Family Cites Families (131)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3106578A (en) | 1960-09-16 | 1963-10-08 | Smith Kline French Lab | Nu-phenethyl-2-phenylcyclopropylamine derivatives |
US3365458A (en) | 1964-06-23 | 1968-01-23 | Aldrich Chem Co Inc | N-aryl-n'-cyclopropyl-ethylene diamine derivatives |
US3532749A (en) | 1965-05-11 | 1970-10-06 | Aldrich Chem Co Inc | N'-propargyl-n**2-cyclopropyl-ethylenediamines and the salts thereof |
US3532712A (en) | 1967-09-29 | 1970-10-06 | Aldrich Chem Co Inc | N'-cyclopropyl ethylenediamine derivatives |
US3471522A (en) | 1967-09-29 | 1969-10-07 | Aldrich Chem Co Inc | N-cyclopropyl-n'-furfuryl-n'-methyl ethylene diamines |
US3654306A (en) | 1970-01-26 | 1972-04-04 | Robins Co Inc A H | 5-azaspiro(2.4)heptane-4 6-diones |
US3758684A (en) | 1971-09-07 | 1973-09-11 | Burroughs Wellcome Co | Treating dna virus infections with amino purine derivatives |
US4530901A (en) | 1980-01-08 | 1985-07-23 | Biogen N.V. | Recombinant DNA molecules and their use in producing human interferon-like polypeptides |
US4409243A (en) | 1981-11-09 | 1983-10-11 | Julian Lieb | Treatment of auto-immune and inflammatory diseases |
US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
GB9311282D0 (en) | 1993-06-01 | 1993-07-21 | Rhone Poulenc Rorer Ltd | New compositions of matter |
AU709303B2 (en) | 1994-10-21 | 1999-08-26 | Nps Pharmaceuticals, Inc. | Calcium receptor-active compounds |
US5652258A (en) | 1995-05-30 | 1997-07-29 | Gliatech, Inc. | 2-(4-imidazoyl) cyclopropyl derivatives |
US20040132820A1 (en) | 1996-02-15 | 2004-07-08 | Jean Gosselin | Agents with leukotriene B4-like antiviral (DNA) and anti-neoplastic activities |
GB9615730D0 (en) | 1996-07-26 | 1996-09-04 | Medical Res Council | Anti-viral agent 1 |
US5961987A (en) | 1996-10-31 | 1999-10-05 | University Of Iowa Research Foundation | Ocular protein stimulants |
DE19647615A1 (en) | 1996-11-18 | 1998-05-20 | Bayer Ag | Process for the preparation of cyclopropylamines |
AR017014A1 (en) | 1997-07-22 | 2001-08-22 | Astrazeneca Ab | TRIAZOL COMPOUNDS [4,5-D] PYRIMIDINE, PHARMACEUTICAL COMPOSITIONS, USE OF THE SAME TO PREPARE MEDICATIONS AND PROCESSES FOR THE PREPARATION OF SUCH COMPOUNDS |
SE9702772D0 (en) | 1997-07-22 | 1997-07-22 | Astra Pharma Prod | Novel compounds |
WO1999031072A1 (en) | 1997-12-18 | 1999-06-24 | E.I. Du Pont De Nemours And Company | Cyclohexylamine arthropodicides and fungicides |
US6809120B1 (en) | 1998-01-13 | 2004-10-26 | University Of Saskatchewan Technologies Inc. | Composition containing propargylamine for enhancing cancer therapy |
PL191832B1 (en) * | 1998-01-16 | 2006-07-31 | Medivir Ab | Antiviral agents |
PL199747B1 (en) | 1998-04-21 | 2008-10-31 | Micromet Ag | CD19xCD3 SPECIFIC POLYPEPTIDES AND USES THEREOF |
SE9802206D0 (en) | 1998-06-22 | 1998-06-22 | Astra Pharma Inc | Novel compounds |
GB2344337A (en) | 1998-12-02 | 2000-06-07 | Fcp | Carton having a rim |
TWI229674B (en) | 1998-12-04 | 2005-03-21 | Astra Pharma Prod | Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses |
ES2237576T3 (en) | 2000-05-26 | 2005-08-01 | Schering Corporation | ADENOSINE A2A RECEIVER ANTAGONISTS. |
TWI290549B (en) * | 2000-06-02 | 2007-12-01 | Astrazeneca Ab | Process for the preparation of cyclopropyl carboxylic acid ester and derivatives |
JP2001354563A (en) | 2000-06-09 | 2001-12-25 | Sankyo Co Ltd | Medicine comprising substituted benzylamines |
US8519005B2 (en) | 2000-07-27 | 2013-08-27 | Thomas N. Thomas | Compositions and methods to prevent toxicity of antiinflammatory agents and enhance their efficacy |
EP1193268A1 (en) | 2000-09-27 | 2002-04-03 | Applied Research Systems ARS Holding N.V. | Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein Junkinases |
CA2432222C (en) | 2000-12-21 | 2008-07-29 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
EP1373203A1 (en) | 2001-03-29 | 2004-01-02 | Bristol-Myers Squibb Company | Cyclopropylindole derivatives as selective serotonin reuptake inhibitors |
RU2332415C2 (en) | 2001-04-27 | 2008-08-27 | Вертекс Фармасьютикалз Инкорпорейтед | Pyrazole derivatives, useful as inhibitors of protein kinase |
DE10123163A1 (en) | 2001-05-09 | 2003-01-16 | Gruenenthal Gmbh | Substituted cyclohexane-1,4-diamine derivatives |
US20030008844A1 (en) | 2001-05-17 | 2003-01-09 | Keryx Biopharmaceuticals, Inc. | Use of sulodexide for the treatment of inflammatory bowel disease |
EP1499598A1 (en) | 2002-04-18 | 2005-01-26 | Ucb, S.A. | Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions |
EP1501514B1 (en) | 2002-05-03 | 2012-12-19 | Exelixis, Inc. | Protein kinase modulators and methods of use |
US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
EP1505966A4 (en) | 2002-05-10 | 2006-08-30 | Bristol Myers Squibb Co | 1,1-disubstituted cycloalkyl derivatives as factor xa inhibitors |
US7456222B2 (en) | 2002-05-17 | 2008-11-25 | Sequella, Inc. | Anti tubercular drug: compositions and methods |
US20040033986A1 (en) | 2002-05-17 | 2004-02-19 | Protopopova Marina Nikolaevna | Anti tubercular drug: compositions and methods |
US6951961B2 (en) | 2002-05-17 | 2005-10-04 | Marina Nikolaevna Protopopova | Methods of use and compositions for the diagnosis and treatment of infectious disease |
WO2004032827A2 (en) | 2002-05-20 | 2004-04-22 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
US7611704B2 (en) | 2002-07-15 | 2009-11-03 | Board Of Regents, The University Of Texas System | Compositions and methods for treating viral infections using antibodies and immunoconjugates to aminophospholipids |
SE0202539D0 (en) | 2002-08-27 | 2002-08-27 | Astrazeneca Ab | Compounds |
DE60318891T2 (en) | 2002-12-13 | 2009-01-22 | Smithkline Beecham Corp. | CYCLOPROPYL COMPOUNDS AS CCR5 ANTAGONISTS |
EA011808B1 (en) | 2003-01-08 | 2009-06-30 | Новартис Вэксинес Энд Дайэгностикс, Инк. | Antibacterial agents |
US7223785B2 (en) | 2003-01-22 | 2007-05-29 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
GB0303439D0 (en) | 2003-02-14 | 2003-03-19 | Pfizer Ltd | Antiparasitic terpene alkaloids |
US7186832B2 (en) | 2003-02-20 | 2007-03-06 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
US7414055B2 (en) | 2003-04-24 | 2008-08-19 | Merck & Co., Inc. | Inhibitors of Akt activity |
US7265246B2 (en) | 2003-07-03 | 2007-09-04 | Eli Lilly And Company | Indane derivates as muscarinic receptor agonists |
AU2004270733B2 (en) | 2003-09-11 | 2011-05-19 | Itherx Pharma, Inc. | Cytokine inhibitors |
CA2534312A1 (en) | 2003-09-12 | 2005-03-24 | Applied Research Systems Ars Holding N.V. | Sulfonamide derivatives for the treatment of diabetes |
CN1897950A (en) | 2003-10-14 | 2007-01-17 | 惠氏公司 | Fused-aryl and heteroaryl derivatives and methods of their use |
EP1677799A4 (en) | 2003-10-21 | 2008-09-10 | Merck & Co Inc | Triazolo-pyridazine compounds and derivatives thereof useful in the treatment of neuropathic pain |
US7026339B2 (en) | 2003-11-07 | 2006-04-11 | Fan Yang | Inhibitors of HCV NS5B polymerase |
WO2005058808A1 (en) | 2003-12-15 | 2005-06-30 | Japan Tobacco Inc. | N-substituted-n-sulfonylaminocyclopropane compounds and pharmaceutical use thereof |
CA2551944A1 (en) | 2003-12-15 | 2005-06-30 | Almirall Prodesfarma Ag | 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists |
CN1901971A (en) | 2003-12-15 | 2007-01-24 | 日本烟草产业株式会社 | Cyclopropane compounds and pharmaceutical use thereof |
US7399825B2 (en) | 2003-12-24 | 2008-07-15 | Lipps Binie V | Synthetic peptide, inhibitor to DNA viruses |
EP1756103A2 (en) | 2004-04-26 | 2007-02-28 | Pfizer, Inc. | Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors |
US20090275099A1 (en) | 2004-04-27 | 2009-11-05 | Regents Of The University Of Michigan | Methods and compositions for treating diseases and conditions associated with mitochondrial function |
CN1950326A (en) * | 2004-06-28 | 2007-04-18 | 特瓦药物精化学品股份有限公司 | Process for the optical resolution and recycling of tomoxetine |
DE102004057594A1 (en) | 2004-11-29 | 2006-06-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Substitute pteridine for the treatment of inflammatory diseases |
EP1833981B1 (en) | 2004-12-16 | 2012-04-18 | President and Fellows of Harvard College | Histone demethylation mediated by the nuclear amine oxidase homolog lsd1 |
ATE476970T1 (en) | 2005-02-18 | 2010-08-15 | Universitaetsklinikum Freiburg | CONTROL OF ANDROGEN RECEPTOR-DEPENDENT GENE EXPRESSION BY INHIBITING THE AMINO OXIDASE ACTIVITY OF LYSINE SPECIFIC DEMETHYLASE (LSD1) |
US20060275366A1 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Controlled-release formulation |
WO2007002220A2 (en) | 2005-06-21 | 2007-01-04 | Bristol-Myers Squibb Company | Aminoacetamide acyl guanidines as beta-secretase inhibitors |
EP1741708A1 (en) | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals |
EA019888B1 (en) | 2005-07-25 | 2014-07-30 | Интермьюн, Инк. | Intermediate compound for making macrocyclic inhibitors of hepatitis c virus replication and method of synthesis thereof |
CN101410367A (en) | 2005-08-10 | 2009-04-15 | 约翰·霍普金斯大学 | Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors |
US20090203750A1 (en) | 2005-08-24 | 2009-08-13 | Alan Kozikowski | 5-HT2C Receptor Agonists as Anorectic Agents |
GB0517740D0 (en) | 2005-08-31 | 2005-10-12 | Novartis Ag | Organic compounds |
TW200745067A (en) | 2006-03-14 | 2007-12-16 | Astrazeneca Ab | Novel compounds |
JP5155303B2 (en) | 2006-05-18 | 2013-03-06 | シンジェンタ パーティシペーションズ アクチェンゲゼルシャフト | New microbicide |
US8198301B2 (en) | 2006-07-05 | 2012-06-12 | Hesheng Zhang | Quinazoline and quinoline derivatives as irreversibe protein tyrosine kinase inhibitors |
WO2008011609A2 (en) | 2006-07-20 | 2008-01-24 | Vical Incorporated | Compositions and methods for vaccinating against hsv-2 |
US20080161324A1 (en) | 2006-09-14 | 2008-07-03 | Johansen Lisa M | Compositions and methods for treatment of viral diseases |
US20110092601A1 (en) | 2007-04-13 | 2011-04-21 | The Johns Hopkins University | Lysine-specific demethylase inhibitors |
US7906513B2 (en) | 2007-04-26 | 2011-03-15 | Enanta Pharmaceuticals, Inc. | Hydrazide-containing hepatitis C serine protease inhibitors |
KR101541203B1 (en) | 2007-06-27 | 2015-07-31 | 아스트라제네카 아베 | Pyrazinone derivatives and their use in the treatment of lung diseases |
JP2010535773A (en) | 2007-08-10 | 2010-11-25 | グラクソスミスクライン エルエルシー | Nitrogen-containing bicyclic chemicals for treating viral infections |
RU2539570C2 (en) | 2007-09-17 | 2015-01-20 | Эббви Бахамаз Лтд. | Pyrimidines applicable as anti-infectious agents, and applications thereof |
US20100016262A1 (en) | 2007-10-18 | 2010-01-21 | Yale University | Compositions and methods for reducing hepatotoxicity associated with drug administration and treating non-alcoholic fatty liver disease, non-alcoholic steatohepatitis and associated cirrhosis |
JP5497650B2 (en) | 2007-10-19 | 2014-05-21 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | CCR10 antagonist |
TW200930397A (en) | 2007-12-26 | 2009-07-16 | Shionogi & Co | Glycosylated glycopeptide antibiotic derivatives |
WO2009109991A2 (en) | 2008-01-23 | 2009-09-11 | Sun Pharma Advanced Research Company Ltd., | Novel hydrazide containing tyrosine kinase inhibitors |
EP2238111B1 (en) | 2008-01-28 | 2013-01-16 | Janssen Pharmaceutica NV | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of -secretase (bace) |
RU2010142655A (en) | 2008-03-19 | 2012-04-27 | Ауриммед Фарма, Инк. (Us) | COMPOUND SUITABLE FOR TREATMENT OF DISEASES AND DISORDERS OF THE CENTRAL NERVOUS SYSTEM, AND METHOD FOR ITS OBTAINING |
JP5674635B2 (en) | 2008-03-27 | 2015-02-25 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | Substituted 4-aminocyclohexane derivatives |
WO2010014921A2 (en) | 2008-08-01 | 2010-02-04 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor antagonists and partial agonists |
WO2009145856A1 (en) | 2008-04-16 | 2009-12-03 | Portola Pharmaceuticals, Inc. | 2, 6-diamino-pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors |
JP2011527667A (en) | 2008-06-18 | 2011-11-04 | 武田薬品工業株式会社 | Halo-substituted pyrimidodiazepine |
US8916596B2 (en) | 2008-07-24 | 2014-12-23 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Preventing or treating viral infection using an inhibitor of the LSD1 protein, a MAO inhibitor or an inhibitor of LSD1 and a MAO inhibitor |
US8048887B2 (en) | 2008-09-11 | 2011-11-01 | Bristol-Myers Squibb Company | Compounds for the treatment of hepatitis C |
WO2010043721A1 (en) | 2008-10-17 | 2010-04-22 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
EP2389362B1 (en) * | 2009-01-21 | 2019-12-11 | Oryzon Genomics, S.A. | Phenylcyclopropylamine derivatives and their medical use |
WO2010085749A2 (en) | 2009-01-23 | 2010-07-29 | Northwestern University | Potent and selective neuronal nitric oxide synthase inhibitors with improved membrane permeability |
WO2010099527A1 (en) | 2009-02-27 | 2010-09-02 | Enanta Pharmaceuticals, Inc. | Hepatitis c virus inhibitors |
SG175925A1 (en) | 2009-05-15 | 2011-12-29 | Novartis Ag | Aryl pyridine as aldosterone synthase inhibitors |
US8389580B2 (en) | 2009-06-02 | 2013-03-05 | Duke University | Arylcyclopropylamines and methods of use |
EP2258865A1 (en) | 2009-06-05 | 2010-12-08 | Universitätsklinikum Freiburg | Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer |
WO2010143582A1 (en) | 2009-06-11 | 2010-12-16 | 公立大学法人名古屋市立大学 | Phenylcyclopropylamine derivatives and lsd1 inhibitors |
AU2010284221B2 (en) | 2009-08-18 | 2016-09-22 | Casero, Robert A | (bis) urea and (bis) thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders |
EP2475254A4 (en) | 2009-09-11 | 2013-05-22 | Enanta Pharm Inc | Hepatitis c virus inhibitors |
EP2480528B1 (en) * | 2009-09-25 | 2018-08-29 | Oryzon Genomics, S.A. | Lysine specific demethylase-1 inhibitors and their use |
WO2011042217A1 (en) | 2009-10-09 | 2011-04-14 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
WO2011057262A2 (en) | 2009-11-09 | 2011-05-12 | Evolva Inc. | Treatment of infections with tp receptor antagonists |
US9616058B2 (en) | 2010-02-24 | 2017-04-11 | Oryzon Genomics, S.A. | Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use |
US9186337B2 (en) | 2010-02-24 | 2015-11-17 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae |
US20130197088A1 (en) | 2010-03-12 | 2013-08-01 | Robert A. Casero, JR. | Compositions and Methods for Combinations of Oligoamines with 2-Difluoromethylornithine (DFMO) |
HUE030938T2 (en) | 2010-04-19 | 2017-06-28 | Oryzon Genomics Sa | Lysine specific demethylase-1 inhibitors and their use |
ES2564352T3 (en) | 2010-04-20 | 2016-03-22 | Università Degli Studi Di Roma "La Sapienza" | Tranylcypromine derivatives as histone demethylase inhibitors LSD1 and / or LSD2 |
EP2560939A2 (en) | 2010-04-20 | 2013-02-27 | Actavis Group Ptc Ehf | Novel process for preparing phenylcyclopropylamine derivatives using novel intermediates |
CA2803354A1 (en) | 2010-06-30 | 2012-01-05 | Actavis Group Ptc Ehf | Novel processes for the preparation of phenylcyclopropylamine derivatives and use thereof for preparing ticagrelor |
EP2598480B1 (en) | 2010-07-29 | 2019-04-24 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
WO2012013728A1 (en) * | 2010-07-29 | 2012-02-02 | Oryzon Genomics S.A. | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
US9527805B2 (en) | 2010-09-10 | 2016-12-27 | Robert A. Casero | Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders |
US20130303545A1 (en) | 2010-09-30 | 2013-11-14 | Tamara Maes | Cyclopropylamine derivatives useful as lsd1 inhibitors |
US9061966B2 (en) | 2010-10-08 | 2015-06-23 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
EP2712316A1 (en) | 2011-02-08 | 2014-04-02 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
EP3981395A1 (en) | 2011-02-08 | 2022-04-13 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
SG193241A1 (en) | 2011-03-25 | 2013-10-30 | Glaxosmithkline Ip No 2 Ltd | Cyclopropylamines as lsd1 inhibitors |
WO2012156531A2 (en) | 2011-05-19 | 2012-11-22 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for inflammatory diseases or conditions |
US20140296255A1 (en) | 2011-05-19 | 2014-10-02 | Oryzong Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
EP2768805B1 (en) | 2011-10-20 | 2020-03-25 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
IL264982B (en) | 2011-10-20 | 2022-08-01 | Oryzon Genomics Sa | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
-
2011
- 2011-07-27 WO PCT/EP2011/062949 patent/WO2012013728A1/en active Application Filing
- 2011-07-27 ES ES11749119.1T patent/ES2674747T3/en active Active
- 2011-07-27 CN CN201180047286.3A patent/CN103124724B/en active Active
- 2011-07-27 DK DK11749119.1T patent/DK2598482T3/en active
- 2011-07-27 ME MEP-2018-163A patent/ME03085B/en unknown
- 2011-07-27 CA CA2806008A patent/CA2806008C/en active Active
- 2011-07-27 AU AU2011284688A patent/AU2011284688B2/en active Active
- 2011-07-27 CN CN201510197250.3A patent/CN104892525A/en active Pending
- 2011-07-27 RU RU2013108702A patent/RU2611437C2/en active
- 2011-07-27 TR TR2018/09057T patent/TR201809057T4/en unknown
- 2011-07-27 EP EP11749119.1A patent/EP2598482B1/en active Active
- 2011-07-27 EP EP18165419.5A patent/EP3375775A1/en not_active Withdrawn
- 2011-07-27 JP JP2013521139A patent/JP6054868B2/en active Active
- 2011-07-27 LT LTEP11749119.1T patent/LT2598482T/en unknown
- 2011-07-27 KR KR1020137004877A patent/KR101866858B1/en active IP Right Grant
- 2011-07-27 PT PT117491191T patent/PT2598482T/en unknown
- 2011-07-27 US US13/812,366 patent/US9181198B2/en active Active
- 2011-07-27 RS RS20180684A patent/RS57331B1/en unknown
- 2011-07-27 NO NO11749119A patent/NO2598482T3/no unknown
- 2011-07-27 SI SI201131504T patent/SI2598482T1/en unknown
- 2011-07-27 MX MX2013000968A patent/MX341732B/en active IP Right Grant
- 2011-07-27 HU HUE11749119A patent/HUE037937T2/en unknown
- 2011-07-27 PL PL11749119T patent/PL2598482T3/en unknown
-
2013
- 2013-01-24 IL IL224389A patent/IL224389A/en active IP Right Grant
-
2015
- 2015-09-09 US US14/848,649 patent/US9708309B2/en active Active
-
2016
- 2016-09-23 JP JP2016186185A patent/JP2017039740A/en active Pending
-
2017
- 2017-06-15 US US15/623,866 patent/US10233178B2/en active Active
-
2018
- 2018-06-12 HR HRP20180916TT patent/HRP20180916T1/en unknown
- 2018-06-22 CY CY181100649T patent/CY1120586T1/en unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20180916T1 (en) | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use | |
JP2013535460A5 (en) | ||
HRP20100677T1 (en) | Imidazo[1,2-a]pyridine compounds as vegf-r2 inhibitors | |
JP2016506960A5 (en) | ||
IL264982B (en) | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors | |
RU2008146995A (en) | N- (2-THIAZOLYL) AMIDE DERIVATIVES AS GSK-3 INHIBITORS | |
JP2019517487A5 (en) | ||
MY148375A (en) | Delta and epsilon crystal forms of imatinib mesylate | |
JP2012507566A5 (en) | ||
JP2017533968A5 (en) | ||
JP2008516986A5 (en) | ||
HRP20140156T1 (en) | N-(hetero)aryl,2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators | |
JP2017538785A5 (en) | ||
JP2016506962A5 (en) | ||
JP2013533879A5 (en) | ||
RU2017126128A (en) | CONDENSED Bicyclic Compounds for the Treatment of Disease | |
GEP20156389B (en) | Oxazolidin-2-one compounds and their usage as pi3ks inhibitors | |
JP2013530176A5 (en) | ||
BRPI0820112B8 (en) | isoxazole-pyridine derivatives, their use and preparation and drug processes | |
JP2010031025A5 (en) | ||
RU2013143028A (en) | Thiazolylphenylbenzenesulfonamide derivatives as kinase inhibitors | |
JP2016506961A5 (en) | ||
BR112012001031A8 (en) | SPIRO AMINO COMPOUNDS SUITABLE FOR THE TREATMENT OF INTER ALIA SLEEP DISORDERS AND DRUG ADDICTION | |
JP2020502092A5 (en) | ||
JP2014510147A5 (en) |